JAK-3激酶及其抑制剂的研究进展

发布时间：2018-03-31 04:21

  本文选题：酪氨酸蛋白激酶　切入点：JAK-　出处：《药学学报》2016年10期

【摘要】：JAK-3激酶(Janus kinase 3)作为酪氨酸蛋白激酶家族成员,在JAK-STAT(Janus kinase-signal transducer and activator of transcription)信号通路中起着非常重要的作用,研究证实JAK-3活性的调控在多种疾病的治疗中起着关键作用,针对该激酶的抑制剂已经有许多相关研究,并有多个JAK-3激酶抑制剂进入临床研究,表现出很好的JAK-3选择性和抑制活性,其中tofacitinib等抑制剂已经通过临床试验,被批准用于类风湿性关节炎的治疗。很多JAK-3抑制剂表现出良好抑制活性的同时,伴有一定的不良反应,有待于改进。本文综述了JAK-3激酶的结构功能以及JAK-3激酶抑制剂的研究进展,为后续研究提供参考。
[Abstract]:JAK-3 kinase Janus kinase 3, as a member of tyrosine protein kinase family, plays a very important role in the JAK-STAT(Janus kinase-signal transducer and activator of transcription.Study shows that the regulation of JAK-3 activity plays a key role in the treatment of many diseases. There have been many related studies on the inhibitors of this kinase, and many JAK-3 kinase inhibitors have entered clinical studies, showing good JAK-3 selectivity and inhibitory activity. Among them, tofacitinib and other inhibitors have passed the clinical trials. Approved for the treatment of rheumatoid arthritis. Many JAK-3 inhibitors exhibit good inhibitory activity with some adverse reactions. The structure and function of JAK-3 kinase and the research progress of JAK-3 kinase inhibitor are reviewed in this paper.
【作者单位】： 中国药科大学药物科学研究院;中国医学科学院北京协和医学院药物研究所;
【基金】：国家自然科学基金资助项目(81573445;81172934)
【分类号】：R96
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本文编号：1689125